G protein-coupled bile acid receptor
|G protein-coupled bile acid receptor 1|
|Symbols||GPBAR1 (; BG37; GPCR19; GPR131; M-BAR; TGR5)|
|External IDs||IUPHAR: ChEMBL: GeneCards:|
|RNA expression pattern|
The G protein-coupled bile acid receptor 1 (GPBAR1) also known G-protein coupled receptor 19 (GPCR19), membrane-type receptor for bile acids (M-BAR) or TGR5 as is a protein that in humans is encoded by the GPBAR1 gene.
This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. This protein functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids.
One effect of this receptor is to activate deiodinases which convert the prohormone thyroxine (T4) to the active hormone triiodothyronine (T3). T3 in turn activates the thyroid hormone receptor which increases metabolic rate.
- Kawamata Y, Fujii R, Hosoya M, Harada M, Yoshida H, Miwa M, Fukusumi S, Habata Y, Itoh T, Shintani Y, Hinuma S, Fujisawa Y, Fujino M (2003). "A G protein-coupled receptor responsive to bile acids". J. Biol. Chem. 278 (11): 9435–40. doi:10.1074/jbc.M209706200. PMID 12524422.
- "Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1".
- Watanabe M, Houten SM, Mataki C, Christoffolete MA, Kim BW, Sato H, Messaddeq N, Harney JW, Ezaki O, Kodama T, Schoonjans K, Bianco AC, Auwerx J (2006). "Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation". Nature 439 (7075): 484–9. doi:10.1038/nature04330. PMID 16400329.
- Baxter JD, Webb P (2006). "Metabolism: bile acids heat things up". Nature 439 (7075): 402–3. doi:10.1038/439402a. PMID 16437098.
- "Bile Acid Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- GPBAR1 protein, human at the US National Library of Medicine Medical Subject Headings (MeSH)
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